Results 21 to 30 of about 588,311 (310)

A TNFR2-Specific TNF Fusion Protein With Improved In Vivo Activity

Frontiers in Immunology, 2022
Tumor necrosis factor (TNF) receptor-2 (TNFR2) has attracted considerable interest as a target for immunotherapy. Indeed, using oligomeric fusion proteins of single chain-encoded TNFR2-specific TNF mutants (scTNF80), expansion of regulatory T cells and ...
Juan Gamboa Vargas, Juan Gamboa Vargas, Jennifer Wagner, Haroon Shaikh, Haroon Shaikh, Isabell Lang, Juliane Medler, Mohamed Anany, Mohamed Anany, Tim Steinfatt, Josefina Peña Mosca, Josefina Peña Mosca, Stephanie Haack, Julia Dahlhoff, Maike Büttner-Herold, Carolin Graf, Estibaliz Arellano Viera, Hermann Einsele, Harald Wajant, Andreas Beilhack, Andreas Beilhack   +20 more
doaj   +1 more source

Analogs of 6-Bromohypaphorine with Increased Agonist Potency for α7 Nicotinic Receptor as Anti-Inflammatory Analgesic Agents

Marine Drugs, 2023
Hypaphorines, tryptophan derivatives, have anti-inflammatory activity, but their mechanism of action was largely unknown. Marine alkaloid L-6-bromohypaphorine with EC50 of 80 μM acts as an agonist of α7 nicotinic acetylcholine receptor (nAChR) involved ...
Igor A. Ivanov, Andrei E. Siniavin, Victor A. Palikov, Dmitry A. Senko, Irina V. Shelukhina, Lyubov A. Epifanova, Lucy O. Ojomoko, Svetlana Y. Belukhina, Nikita A. Prokopev, Mariia A. Landau, Yulia A. Palikova, Vitaly A. Kazakov, Natalia A. Borozdina, Arina V. Bervinova, Igor A. Dyachenko, Igor E. Kasheverov, Victor I. Tsetlin, Denis S. Kudryavtsev   +17 more
doaj   +1 more source

⁶⁸Ga-Labeled [Thz¹⁴]Bombesin(7–14) Analogs: Promising GRPR-Targeting Agonist PET Tracers with Low Pancreas Uptake

Molecules, 2023
With overexpression in various cancers, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer imaging and therapy. However, the high pancreas uptake of reported GRPR-targeting radioligands limits their clinical application.
Lei Wang, Ivica Jerolim Bratanovic, Zhengxing Zhang, Hsiou-Ting Kuo, Helen Merkens, Jutta Zeisler, Chengcheng Zhang, Ruiyan Tan, François Bénard, Kuo-Shyan Lin   +9 more
doaj   +1 more source

High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist

Molecules, 2021
Relaxin/insulin-like family peptide receptor 3 (RXFP3) belongs to class A G protein-coupled receptor family. RXFP3 and its endogenous ligand relaxin-3 are mainly expressed in the brain with important roles in the regulation of appetite, energy metabolism,
Guangyao Lin, Yang Feng, Xiaoqing Cai, Caihong Zhou, Lijun Shao, Yan Chen, Linhai Chen, Qing Liu, Qingtong Zhou, Ross A.D. Bathgate, Dehua Yang, Ming-Wei Wang   +11 more
doaj   +1 more source

Structural Probing and Molecular Modeling of the A3 Adenosine Receptor: A Focus on Agonist Binding

Molecules, 2017
Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, termed A1, A2A, A2B and A3, which belong to the G protein-coupled receptor (GPCR) superfamily.
Antonella Ciancetta, Kenneth A. Jacobson
doaj   +1 more source

Synthetic Studies on the Indane SHIP1 Agonist AQX-1125. [PDF]

, 2021
A new synthetic route to the SHIP1 agonist AQX-1125 has been developed. This sequence utilizes a hydroxy-acid intermediate which allows for ready differentiation of the C6 and C7 positions.
Shawn, Dormann, William, Kerr, Otto, Dungan, Daniel, Effiong, John, Chisholm, Sandra, Fernandes-Denney, Brian, Duffy   +6 more
core   +2 more sources

On agonistic memory [PDF]

Memory Studies, 2016
Building on Mouffe’s critique of cosmopolitanism, this article argues that a cosmopolitan mode of remembering, far from having superseded the antagonistic mode associated with ‘first modernity’ in the European context, has proved unable to prevent the rise of, and is being increasingly challenged by, new antagonistic collective memories constructed by
Cento Bull, Anna, Hansen, Hans Lauge
openaire   +3 more sources

Licraside as novel potent FXR agonist for relieving cholestasis: structure-based drug discovery and biological evaluation studies

Frontiers in Pharmacology, 2023
Cholestasis is a common clinical disease caused by a disorder in bile acids (BAs) homeostasis, which promotes its development. The Farnesoid X receptor (FXR) plays a critical role in regulating BAs homeostasis, making it an essential target for ...
Lili Xi, Axi Shi, Tiantian Shen, Guoxu Wang, Yuhui Wei, Jingjing Guo   +5 more
doaj   +1 more source

Agonist-Dependent Coupling of the Promiscuous Adenosine A_2B Receptor to Gα Protein Subunits

, 2022
The adenosine A2B receptor (A2BAR) belongs to the rhodopsin-like G protein-coupled receptor (GPCR) family. It is upregulated under hypoxic conditions, in inflammation and cancer.
Asuka Inoue, Asuka Inoue (52011), Andhika B. Mahardhika, Christa E. Müller (1550497), Christa E. Müller, Jan Hendrik Voss, Jan Hendrik Voss (12493780), Andhika B. Mahardhika (6400748)   +7 more
core   +1 more source

Immune Checkpoints as Therapeutic Targets in Autoimmunity

Frontiers in Immunology, 2018
Antibodies that block the immune checkpoint receptors PD1 and CTLA4 have revolutionized the treatment of melanoma and several other cancers, but in the process, a new class of drug side effect has emerged—immune related adverse events.
Christopher Paluch, Christopher Paluch, Ana Mafalda Santos, Ana Mafalda Santos, Consuelo Anzilotti, Consuelo Anzilotti, Richard J. Cornall, Richard J. Cornall, Simon J. Davis, Simon J. Davis   +9 more
doaj   +1 more source